939375-07-2Relevant academic research and scientific papers
Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes
Qian, Yimin,Wertheimer, Stanley J.,Ahmad, Mushtaq,Cheung, Adrian Wai-Hing,Firooznia, Fariborz,Hamilton, Matthew M.,Hayden, Stuart,Li, Shiming,Marcopulos, Nicholas,McDermott, Lee,Tan, Jenny,Yun, Weiya,Guo, Liang,Pamidimukkala, Anjula,Chen, Yingsi,Huang, Kuo-Sen,Ramsey, Gwendolyn B.,Whittard, Toni,Conde-Knape, Karin,Taub, Rebecca,Rondinone, Cristina M.,Tilley, Jefferson,Bolin, David
experimental part, p. 2433 - 2446 (2011/06/17)
Diacylglycerol acyltransferase-1 (DGAT-1) is the enzyme that catalyzes the final and committed step of triglyceride formation, namely, the acylation of diacylglycerol with acyl coenzyme A. DGAT-1 deficient mice demonstrate resistance to weight gain on hig
Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors
Yun, Weiya,Ahmad, Mushtaq,Chen, Yingsi,Gillespie, Paul,Conde-Knape, Karin,Kazmer, Sonja,Li, Shiming,Qian, Yimin,Taub, Rebecca,Wertheimer, Stanley J.,Whittard, Toni,Bolin, David
scheme or table, p. 7205 - 7209 (2012/01/15)
In a discovery effort to find safe and effective DGAT-1 inhibitors, we have identified 2-phenyloxazole 4-carboxamide 1 as a conformationally constrained analog of a hydrazide hit, which was previously identified from high-throughput screening. Further optimization of this series has led to chemically more stable 2-phenyloxazole-based DGAT-1 inhibitor 25 with improved solubility, cell-based activity, and pharmacokinetic properties. Compound 25 also demonstrated in vivo efficacy in a diet-induced obesity (DIO) rat model.
Diacylglycerol acyltransferase inhibitors
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Page/Page column 36, (2010/11/27)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
